For prophylaxis and treatment of myocardial infarction a wide range of well-known preparations is used, namely: organic nitrates and nitrites, .beta.-adreno-blockers, analgetic agents, anticoagulating and fibrinolytic agents, antiarrhythmic and cardiotonic preparations and, quite recently, calcium antagonists.
To reduce the arterial pressure and lower the heart load, preparations with different mechanisms of action are used. Neurotropic hypotensive preparations affect various units of the nervous regulation: cholinolytic preparations lower the muscular tension of the organs having cholinergic innervation, antiadrenergic preparations lower the tension of a number of organs and systems having adrenergic innervation. However, it is rather difficult to administer such preparations in the case of an acute cardiac insufficiency, as well as in the post-infarction state.
Preparations of a central sedative effect (sedatives, tranquilizers, soporific agents) restrict the flow of efferent nervous pulses, thus resulting in a reduced arterial pressure and a lowered oxygen demand of the heart. However, their protracted administration is accompanied by the development of adaptation and narcomania. Ganglioblockers, while inhibiting propagation of excitation in sympathetic and parasympathetic ganglia, exert a hypotensive effect, but their administration is contraindicated in the case of an accute heart insufficiency and post-infarction state.
Known are various .beta.-adrenoblockers such as inderal, benzodixin, oxyprenolol; they, however, feature a number of side phenomena. These preparations are toxic (LD.sub.50 for inderal is 30 to 50 mg/kg for white mice). They also have a negative inotropic effect; contraindicated for a number of cardiac diseases such as sinus bradycardia, bronchial asthma and the like; they can also cause allergic responses.
Among calcium antagonists an evergrowing use enjoys the preparation nifedipine. However, its effect likewise that of other preparations of this group, is not sufficiently long (no longer than 8 hours) which necessitates a three-times daily administration thereof. Furthermore, discontinuation of the administration of the preparation results in a recurrence of hypertension and a higher consumption of oxygen.
Also known in the art is a naturally-occurring alkaloid stachydrine (1,1-dimethylpyrrolidin-1-io-2-yl)formate (cf. Rodina L. G., Determination of the Pharmacological Effect of Some Components of Leonorus Guingulobatus, Pharmacia, 1968, 17 (2), 55-58).
This alkaloid is recovered from Leonorus extract and has a hypotensive effect. This compound, however, considerably lowers the number of cardiac contractions (by 19% on the average), thus substantially limiting the possibilities of its application. Furthermore, stachydrine sharply changes the blood coagulability.
Known in the art is a compound-(1,1-diemthyl-3-oxopyrazolidin-1-io-4-yl)acetate (cf. L. K. Dalton, S. Demeral, B. S. Elmes. The reactions of some 1,1-dialkylhydrazines with unsaturated and bromoaliphatic acids, Aust. J. Chem., 1980, 17(2), 55-58).
Biological activity of this compound has not been hitherto described in the literature.